公开(公告)号：US20240182519A1

公开(公告)日：2024-06-06

申请号：US18142621

申请日：2023-05-03

申请人： IPSEN PHARMA S.A.S.

发明人： Zheng Xin Dong ,  Daniel B. Deoliveira ,  Jeanne Mary Comstock

IPC分类号： C07K7/06 ,  C07K7/56 ,  C07K14/68

CPC分类号： C07K7/06 ,  C07K7/56 ,  C07K14/68 ,  A61K38/00

摘要： The present invention relates to peptide ligands of the melanocortin receptors, in particular the melanocortin-4 receptor, and as such, are useful in the treatment of disorders responsive to the activation of this receptor, such as obesity, diabetes mellitus and sexual dysfunction.

公开(公告)号：US09814755B2

公开(公告)日：2017-11-14

申请号：US14943936

申请日：2015-11-17

申请人： THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA

发明人： Victor J. Hruby ,  Minying Cai ,  Horst Kessler

IPC分类号： C07K14/68 ,  C07K7/06 ,  C07K14/685 ,  A61K8/64 ,  A61K38/17 ,  A61K38/12 ,  A61K31/555 ,  A61K38/10 ,  A61K9/00 ,  A61K47/24 ,  A61K9/107 ,  A61K9/70 ,  C07K14/72 ,  C07K7/08

CPC分类号： A61K38/12 ,  A61K9/0014 ,  A61K9/107 ,  A61K9/2004 ,  A61K9/7023 ,  A61K9/7084 ,  A61K31/555 ,  A61K38/10 ,  A61K38/177 ,  A61K47/24 ,  C07K7/08 ,  C07K14/68 ,  C07K14/685 ,  C07K14/723

摘要： Methods of treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising Ac-Nle4-c[Asp5-His6-(NMe)D-Nal(2′)7-Arg8-Trp9-(NMe)Lys10]-NH2 (PEPTIDE 9), in a pharmaceutically acceptable carrier is administered to the subject. PEPTIDE 9 is a selective MC5R antagonist, in which administration thereof to the subject can treat the depressive or generalized anxiety disorder with clinical improvement observed in a relatively short time.

公开(公告)号：US20170218017A1

公开(公告)日：2017-08-03

申请号：US15263028

申请日：2016-09-12

申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. ,  INTEZYNE TECHNOLOGIES INC. ,  ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA ,  BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

发明人： ROBERT J. GILLIES ,  DAVID L. MORSE ,  NATALIE M. BARKEY ,  KEVIN N. SILL ,  JOSEF VAGNER ,  NARGES K. TAFRESHI ,  JONATHAN L. SESSLER ,  CHRISTIAN PREIHS ,  VICTOR J. HRUBY

IPC分类号： C07K5/117 ,  C07K7/08 ,  A61K49/18 ,  C07K7/06

CPC分类号： C07K5/1024 ,  A61K38/34 ,  A61K47/64 ,  A61K47/6907 ,  A61K49/0056 ,  A61K49/101 ,  A61K49/1809 ,  C07K7/08 ,  C07K14/68 ,  C07K14/723

摘要： The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

公开(公告)号：US20170145056A1

公开(公告)日：2017-05-25

申请号：US15422850

申请日：2017-02-02

申请人： Palatin Technologies, Inc.

发明人： Wei Yang ,  Yi-Qun Shi

IPC分类号： C07K7/06

CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K14/68 ,  Y02A50/401

摘要： Melanocortin receptor-specific linear peptides of the formula Z-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Y   (VI) or a pharmaceutically acceptable salt thereof, where Z, Y, Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, and Xaa6 are as defined in the specification, compositions and formulations including peptides of the foregoing formula or salts thereof, and pharmaceutical compositions for preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.

公开(公告)号：US20170020952A1

公开(公告)日：2017-01-26

申请号：US14943885

申请日：2015-11-17

申请人： THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA

发明人： Victor J. Hruby ,  Minying Cai

IPC分类号： A61K38/12

CPC分类号： A61K38/12 ,  A61K9/0014 ,  A61K9/107 ,  A61K9/2004 ,  A61K9/7023 ,  A61K9/7084 ,  A61K38/10 ,  A61K47/24 ,  C07K7/08 ,  C07K14/68 ,  C07K14/685 ,  C07K14/723

摘要： Methods of treating a central nervous system (CNS) disorder or mood disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand in a pharmaceutically acceptable carrier is administered to the subject. The MC5R peptide ligand is a selective MC5R antagonist, in which administration thereof to the subject can treat the CNS disorder or mood disorder with clinical improvement observed in a relatively short time.

摘要翻译： 描述了在需要这种治疗的受试者中治疗中枢神经系统（CNS）障碍或情绪障碍的方法。 向受试者施用治疗有效量的包含药学上可接受的载体中的黑皮质素5受体（MC5R）肽配体的组合物。 MC5R肽配体是选择性MC5R拮抗剂，其中施用于受试者可以在相对短的时间内观察到临床改善来治疗CNS病症或情绪障碍。

公开(公告)号：US20150157747A1

公开(公告)日：2015-06-11

申请号：US14622217

申请日：2015-02-13

申请人： STC.UNM

发明人： Yubin Miao ,  Haixun Guo

IPC分类号： A61K51/08 ,  A61K45/06 ,  C07K7/54

CPC分类号： C07K14/68 ,  A61K38/00 ,  A61K45/06 ,  A61K51/08 ,  A61K51/086 ,  A61K51/088 ,  C07K7/54

摘要： The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

摘要翻译： 本发明涉及用于成像癌症的新型非侵入性诊断工具/化合物，特别是黑素瘤，包括体内转移性黑素瘤。 本发明化合物在癌细胞和组织中表现出增强的摄取，并且减少了肾中的肾摄取，证明了本发明化合物的有利的药代动力学。 根据本发明的化合物代表使用非侵入性分子成像技术在黑色素瘤的诊断和治疗中的进展，包括转移性黑素瘤。 本发明的新型探针也可用于开始黑色素瘤的治疗以及监测患者对化疗治疗的反应和用于治疗黑素瘤/转移性黑色素瘤的其它干预或治疗。 根据本发明的化合物可以用作许多病症和疾病状态的诊断工具以及用于治疗这些病症和疾病状态的治疗剂。

公开(公告)号：US20140135473A1

公开(公告)日：2014-05-15

申请号：US14070367

申请日：2013-11-01

申请人： Aileron Therapeutics, Inc.

发明人： Huw M. Nash

IPC分类号： C07K14/47 ,  C07K1/113

CPC分类号： A61K38/12 ,  C07K1/1133 ,  C07K14/4747 ,  C07K14/68 ,  C07K14/705

摘要： The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.

摘要翻译： 本发明提供新颖的拟肽大环化合物及其制备和使用的方法，以及氨基酸类似物和大环化合物形成接头以及可用于其生产的试剂盒。

公开(公告)号：US20120225816A1

公开(公告)日：2012-09-06

申请号：US13508777

申请日：2010-11-15

申请人： Zheng Xin Dong ,  Jundong Zhang

发明人： Zheng Xin Dong ,  Jundong Zhang

IPC分类号： A61K38/12 ,  A61P5/00

CPC分类号： A61K38/33 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/08 ,  A61K38/34 ,  C07K14/68 ,  C07K14/69

摘要： The present invention relates to improvements in compositions containing peptides that are ligands of one or more of the melanocortin receptors (MC-R), or pharmaceutically acceptable salts thereof, methods for preparing such compositions, and method of using such compositions to treat mammals. In particular, the present invention relates to a pharmaceutical composition comprising a pamoate salt of Ac-Arg-cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2 which is a ligand of the melanocortin receptor subtype 4 (MC4-R), and in which, after subcutaneous or intramuscular administration to a subject, the peptide forms a depot at physiological pH that is slowly dissolved and released into the body fluid and bloodstream. The present invention may further comprise an organic component such as dimethylacetamide (DMA) or polyethylene glycol (PEG) with an average molecular weight of lower than 1000.

摘要翻译： 本发明涉及包含作为一种或多种黑皮质素受体（MC-R）或其药学上可接受的盐的配体的肽的组合物的改进，以及用于制备该组合物的方法以及使用这些组合物治疗哺乳动物的方法。 特别地，本发明涉及包含作为黑皮质素受体配体的Ac-Arg-环（Cys-D-Ala-His-D-Phe-Arg-Trp-Cys）-NH 2的双羟萘酸盐的药物组合物 亚型4（MC4-R），并且其中在对受试者皮下或肌肉内施用后，肽在生理pH下形成缓慢溶解并释放到体液和血流中的贮库。 本发明还可以包含平均分子量低于1000的有机组分如二甲基乙酰胺（DMA）或聚乙二醇（PEG）。

公开(公告)号：US20110312878A1

公开(公告)日：2011-12-22

申请号：US13027475

申请日：2011-02-15

申请人： Bjarne Due Larsen

发明人： Bjarne Due Larsen

IPC分类号： A61K38/34 ,  C07K1/107 ,  C12P21/00 ,  A61K38/35 ,  A61K38/33 ,  A61P19/10 ,  A61P31/18 ,  A61P35/00 ,  A61P13/00 ,  A61P9/12 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P25/24 ,  A61P5/24 ,  A61P25/18 ,  C07K19/00

CPC分类号： C07K14/665 ,  A61K38/00 ,  A61K47/64 ,  A61K47/65 ,  A61K47/67 ,  B82Y5/00 ,  C07K1/1075 ,  C07K14/575 ,  C07K14/57545 ,  C07K14/675 ,  C07K14/68 ,  C07K14/685 ,  C07K14/695 ,  C07K2319/31

摘要： The invention is directed to a pharmacologically active peptide conjugate having a reduced tendency towards enzymatic cleavage comprising a pharmacologically active peptide sequence (X) and a stabilising peptide sequence (Z) of 4-20 amino acid residues covalently bound to X.

摘要翻译： 本发明涉及具有减少的酶切割趋势的药理学活性肽缀合物，其包含与X共价结合的4-20个氨基酸残基的药理学活性肽序列（X）和稳定肽序列（Z）。

公开(公告)号：US07754691B1

公开(公告)日：2010-07-13

申请号：US11428749

申请日：2006-07-05

申请人： Shubh D. Sharma

发明人： Shubh D. Sharma

IPC分类号： A61K38/07 ,  A61K38/08

CPC分类号： C07K5/1002 ,  A61K38/00 ,  C07K5/1024 ,  C07K7/06 ,  C07K14/68

摘要： Linear peptides with a C-terminus —OH group that are specific for one or more melanocortin receptors, and which may be used in the treatment of melanocortin receptor-mediated disorders, including a variety of body weight disorders including cachexia, and for treatment of inflammation, immune disorders and other conditions, diseases and syndromes, and pharmaceutical compositions including such linear peptides.

摘要翻译： 具有一个或多个黑皮质素受体特异性的C末端-OH基团的线性肽，其可用于治疗黑皮质素受体介导的病症，包括各种体重紊乱（包括恶病质）和治疗炎症 ，免疫疾病和其他病症，疾病和综合征，以及包括这种线性肽的药物组合物。